Investigation of Absorption Routes of Meloxicam and Its Salt Form from Intranasal Delivery Systems

Molecules

Tamás Janáky¹  Ferenc Tömösi¹  Gábor Kecskeméti¹  Róbert Gáspár²  Árpád Márki²  Anita Sztojkov-Ivanov²  Rita Ambrus³  Csilla Bartos³  Piroska Szabó-Révész³  Anita Kovács³ 

[1] Department of Medical Chemistry, University of Szeged, Dóm tér 8, H-6720 Szeged, Hungary;Department of Pharmacodynamics and Biopharmacy, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary;Institute of Pharmaceutical Technology and Regulatory Affairs, University of Szeged, Eötvös u. 6, H-6720 Szeged, Hungary;

关键词: nanosized meloxicam;    meloxicam potassium monohydrate;    intranasal formulation;    dissolution rate;    in vitro diffusion;    plasma drug-content;    absolute bioavailability for brain;   

DOI  :  10.3390/molecules23040784

来源: DOAJ

【 摘 要 】

The aim of this article was to study the trans-epithelial absorption to reach the blood and to target the brain by axonal transport using nasal formulations with nanonized meloxicam (nano MEL spray) and its salt form known as meloxicam potassium monohydrate (MELP spray). The physicochemical properties and the mucoadhesivity of nasal formulations were controlled. In vitro and in vivo studies were carried out. These forms were first investigated in “nose-to-brain” relation. It was found that the in vitro study and in vivo study did not show any significant correlation. In vitro experiments demonstrated faster dissolution rate and higher diffusion of MELP from the spray compared with the nano MEL spray. The administration of the nano MEL spray resulted in faster absorption and constant plasma concentration of the drug after five minutes of administration as compared to MELP. The axonal transport of the drug was justified. MEL appeared in the brain tissues after the first five minutes of administration in the case of both spray forms, but its amount was too small in comparison with the total plasma concentration. The application of the nano MEL spray resulted in the same AUC in the brain as the intravenous injection. The “nose-to-blood” results predicted the nasal applicability of MEL and MELP in pain management. The “nose-to-brain” pathway requires further study.

【 授权许可】

Unknown